Comparison of binding affinities and calcium current inhibitory effects of a 1,4-dihydropyridine derivative (PN 200-110) in vascular smooth muscle. 1988

C Dacquet, and P Pacaud, and G Loirand, and C Mironneau, and J Mironneau
Laboratoire de Physiologie Cellulaire et Pharmacologie Moléculaire, I.B.C.N. du C.N.R.S., Université Bordeaux II, France.

The binding of (+) (3H) PN 200-110 to high and low affinity sites in mammalian portal vein smooth muscle membranes was characterized. Binding affinities were 0.09 and 30 nM for the high and low affinity sites, respectively, and binding site densities were 45 and 400 fmoles/mg of protein for the respective sites. (+) PN 200-110 blocked both fast and slow calcium currents in isolated cells from portal vein smooth muscle. The blockade of slow calcium current was voltage-dependent as PN 200-110 bound with higher affinity to inactivated slow calcium channels (IC50 = 0.03 nM) than to resting channels (IC50 = 0.15 nM). The blockade of fast calcium current was voltage-independent (IC50 = 45 nM). The IC50 values found from electrophysiological experiments for the binding to inactivated slow and fast calcium channels are similar to the Kd values determined by radioligand binding.

UI MeSH Term Description Entries
D007700 Kinetics The rate dynamics in chemical or physical systems.
D009131 Muscle, Smooth, Vascular The nonstriated involuntary muscle tissue of blood vessels. Vascular Smooth Muscle,Muscle, Vascular Smooth,Muscles, Vascular Smooth,Smooth Muscle, Vascular,Smooth Muscles, Vascular,Vascular Smooth Muscles
D009529 Nicardipine A potent calcium channel blockader with marked vasodilator action. It has antihypertensive properties and is effective in the treatment of angina and coronary spasms without showing cardiodepressant effects. It has also been used in the treatment of asthma and enhances the action of specific antineoplastic agents. Antagonil,Cardene,Cardene I.V.,Cardene SR,Dagan,Flusemide,Lecibral,Lincil,Loxen,Lucenfal,Nicardipine Hydrochloride,Nicardipine LA,Nicardipino Ratiopharm,Nicardipino Seid,Perdipine,Ridene,Vasonase,Y-93,Hydrochloride, Nicardipine,LA, Nicardipine,Y 93,Y93
D010069 Oxadiazoles Compounds containing five-membered heteroaromatic rings containing two carbons, two nitrogens, and one oxygen atom which exist in various regioisomeric forms. Oxadiazole
D002118 Calcium A basic element found in nearly all tissues. It is a member of the alkaline earth family of metals with the atomic symbol Ca, atomic number 20, and atomic weight 40. Calcium is the most abundant mineral in the body and combines with phosphorus to form calcium phosphate in the bones and teeth. It is essential for the normal functioning of nerves and muscles and plays a role in blood coagulation (as factor IV) and in many enzymatic processes. Coagulation Factor IV,Factor IV,Blood Coagulation Factor IV,Calcium-40,Calcium 40,Factor IV, Coagulation
D004594 Electrophysiology The study of the generation and behavior of electrical charges in living organisms particularly the nervous system and the effects of electricity on living organisms.
D006736 Horses Large, hoofed mammals of the family EQUIDAE. Horses are active day and night with most of the day spent seeking and consuming food. Feeding peaks occur in the early morning and late afternoon, and there are several daily periods of rest. Equus caballus,Equus przewalskii,Horse, Domestic,Domestic Horse,Domestic Horses,Horse,Horses, Domestic
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D001665 Binding Sites The parts of a macromolecule that directly participate in its specific combination with another molecule. Combining Site,Binding Site,Combining Sites,Site, Binding,Site, Combining,Sites, Binding,Sites, Combining
D013237 Stereoisomerism The phenomenon whereby compounds whose molecules have the same number and kind of atoms and the same atomic arrangement, but differ in their spatial relationships. (From McGraw-Hill Dictionary of Scientific and Technical Terms, 5th ed) Molecular Stereochemistry,Stereoisomers,Stereochemistry, Molecular,Stereoisomer

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